Hafez Hend N, El-Gazzar Abdel-Rhman B A, Al-Hussain Sami A
Al-Imam Mohammad Ibn Saud Islamic University (IMSIU), College of Science, Department of Chemistry, P.O. Box: 90950, Riyadh 11623, Saudi Arabia; Photochemistry Department (Heterocyclic & Nucleosides Unit), National Research Centre, Dokki, Giza 12622, Egypt.
Al-Imam Mohammad Ibn Saud Islamic University (IMSIU), College of Science, Department of Chemistry, P.O. Box: 90950, Riyadh 11623, Saudi Arabia.
Bioorg Med Chem Lett. 2016 May 15;26(10):2428-2433. doi: 10.1016/j.bmcl.2016.03.117. Epub 2016 Apr 2.
A series of 4-amino-3-(4-chlorophenyl)-1H-pyrazol-5-yl-methanone and 6-amino-3-(4-chlorophenyl)-5-methyl-1,6-dihydro-7H-pyrazolo[4,3-d]-pyrimidin-7-one have been synthesized from ethyl 4-amino-3-(4-chlorophenyl)-pyrazol-5-carboxylate. The newly synthesized compounds were characterized by IR, (1)H NMR, (13)CNMR, Mass spectra and Elemental analysis. The compounds were evaluated for their in vitro antimicrobial and anticancer activity. Among the synthesized compounds, compounds 7a,b and 15 exhibited higher anticancer activity than the doxorubicin as reference drug. Most of the newly synthesized compounds have good to excellent antimicrobial activity.
由4-氨基-3-(4-氯苯基)-1H-吡唑-5-羧酸乙酯合成了一系列4-氨基-3-(4-氯苯基)-1H-吡唑-5-基甲酮和6-氨基-3-(4-氯苯基)-5-甲基-1,6-二氢-7H-吡唑并[4,3-d]嘧啶-7-酮。通过红外光谱、核磁共振氢谱、核磁共振碳谱、质谱和元素分析对新合成的化合物进行了表征。对这些化合物的体外抗菌和抗癌活性进行了评估。在合成的化合物中，化合物7a、b和15表现出比作为参考药物的阿霉素更高的抗癌活性。大多数新合成的化合物具有良好至优异的抗菌活性。
